Identification

Name
Lindane
Accession Number
DB00431  (APRD01072)
Type
Small Molecule
Groups
Approved, Withdrawn
Description

An organochlorine insecticide that has been used as a pediculicide and a scabicide. Lindane has been banned in California, United Kingdom, Australia, and many western countries due to concerns about neurotoxicity and adverse effects on the environment. In Canada, Lindane is not recommmended as a first-line therapy due to reports of resistance, neurotoxicity, and bone marrow suppression, but has been approved by the FDA as a second-line therapy for topical treatment of pediculosis capitis (head lice), pediculosis pubis (pubic lice), or scabies in patients greater than two years of age who cannot tolerate or have failed first-line treatment. Lindane is still allowed for pharmaceutical use until 2015.

Structure
Thumb
Synonyms
  • (1alpha,2alpha,3beta,4alpha,5alpha,6beta)-1,2,3,4,5,6-Hexachlorocyclohexane
  • (1R,2c,3t,4c,5c,6t)-1,2,3,4,5,6-Hexachlorocyclohexane
  • 1,2,3,4,5,6-Hexachlorocyclohexane
  • Benzene hexachloride
  • gamma-1,2,3,4,5,6-Hexachlorocyclohexane
  • gamma-Benzene hexachloride
  • gamma-BHC
  • gamma-HCH
  • gamma-Hexachlorocyclohexane
  • gamma-Hexachlorzyklohexan
  • gamma-Lindane
  • Gammallin
  • Gammaxene
  • Lindan
  • γ-hexachlorocyclohexane
  • γ-Hexachlorzyklohexan
  • γ-lindane
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LindaneLotion10 mg/mLTopicalMorton Grove Pharmaceuticals, Inc.1984-08-162017-11-16Us
LindaneShampoo10 mg/mLTopicalVersa Pharm Incorporated2011-11-21Not applicableUs
LindaneShampoo10 mg/mLTopicalMorton Grove Pharmaceuticals, Inc.1994-12-12Not applicableUs
LindaneLotion10 mg/mLTopicalVersa Pharm Incorporated2011-12-05Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dom-lindane Lotion - 1%Liquid1 %TopicalDominion Pharmacal1995-12-312004-08-16Canada
Hexit LotionLotion1 %TopicalOdan Laboratories Ltd2003-07-152012-12-31Canada
Hexit Shampoo 1.0%Shampoo1 %TopicalOdan Laboratories Ltd1989-12-312012-12-31Canada
Kwellada Lotion 1%Lotion1 %TopicalReed & Carnrick, Division Of Block Drug Company (Canada) Ltd.1958-12-311997-07-22Canada
Kwellada Shampoo 1%Shampoo1 %TopicalReed & Carnrick, Division Of Block Drug Company (Canada) Ltd.1960-12-311997-07-22Canada
Lindane Lotion USP 1%Lotion1 %TopicalNational Care Products Ltd.1996-08-272002-10-10Canada
Lindane Shampoo USP 1%Shampoo1 %TopicalNational Care Products Ltd.1994-12-312001-10-05Canada
PMS-lindane Lot 1%Lotion1 %TopicalPharmascience Inc1987-12-312012-07-20Canada
PMS-lindane Shp 1%Shampoo1 %TopicalPharmascience Inc1987-12-312012-04-16Canada
International/Other Brands
Gamene / Kwell / Scabene
Categories
UNII
59NEE7PCAB
CAS number
58-89-9
Weight
Average: 290.83
Monoisotopic: 287.860066434
Chemical Formula
C6H6Cl6
InChI Key
JLYXXMFPNIAWKQ-GNIYUCBRSA-N
InChI
InChI=1S/C6H6Cl6/c7-1-2(8)4(10)6(12)5(11)3(1)9/h1-6H/t1-,2-,3-,4+,5+,6+
IUPAC Name
(1R,2S,3r,4R,5S,6r)-1,2,3,4,5,6-hexachlorocyclohexane
SMILES

Pharmacology

Indication

For the treatment of patients infested with Sarcoptes scabiei or pediculosis capitis who have either failed to respond to adequate doses, or are intolerant of other approved therapies.

Structured Indications
Pharmacodynamics

Scabies is a common, highly pruritic infestation of the skin caused by Sarcoptes scabiei (lice). It is a very contagious condition with specific lesions, such as burrows, and nonspecific lesions, such as papules, vesicles and excoriations. The typical areas of the body it affects are finger webs, scalp (hair), wrists, axillary folds, abdomen, buttocks, inframammary folds and genitalia (males). It is characterized by intense night-time itching. Scabies is spread through close personal contact (relatives, sexual partners, schoolchildren, chronically ill patients and crowded communities). Scabies infestations and the corresponding symptoms can be eliminated by killing the scabies with topical insecticides or scabicides. Lindane is a scabicide that is essentially an organochloride insecticide.

Mechanism of action

Lindane is an organochloride insecticide that has similar neurotoxic protperties to DDT. It exerts its parasiticidal action by being directly absorbed through the parasite's exoskeleton (primarily lice, or scabies) and their ova. The gamma-aminobutyric acid (GABA(1)) receptor/chloride ionophore complex is the primary site of action for lindane, and other insecticides such as endosulfan, and fipronil. Blockage of the GABA-gated chloride channel reduces neuronal inhibition, which leads to hyperexcitation of the central nervous system. This results in paralysis, convulsions, and death. Lindane has very low ovicidal activity.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit beta-1
antagonist
Human
UGlycine receptor subunit alpha-1
antagonist
Human
UGlycine receptor subunit alpha-2
antagonist
Human
UGlycine receptor subunit alpha-3
antagonist
Human
UGlycine receptor subunit beta
antagonist
Human
UGamma-aminobutyric acid receptor subunit beta-3Not AvailableHuman
UGamma-aminobutyric acid receptor subunit rho-1Not AvailableHuman
UProgesterone receptorNot AvailableHuman
UEstrogen receptor alphaNot AvailableHuman
UNuclear receptor subfamily 1 group I member 2Not AvailableHuman
Absorption

Lindane is absorbed significantly through the skin. A mean peak blood concentration of 28 nanograms per mL occurred in infants and children 6 hours after total body application of lindane lotion for scabies.

Volume of distribution
Not Available
Protein binding

91%

Metabolism

Primarily hepatic through dechlorination leading to 2-chlorophenol, 0-chlorophenol, chlorocyclohexane, chlorocyclohexanol.

Route of elimination
Not Available
Half life

18 hours

Clearance
Not Available
Toxicity

Lindane is a moderately toxic compound via oral exposure, with a reported oral LD50 of 88 to 190 mg/kg in rats. Gamma-HCH (which constitutes 99% of lindane) is generally considered to be the most acutely toxic of the isomers following single administration. It is moderately toxic via the dermal route as well, with reported dermal LD50 values of 500 to 1000 mg/kg in rats, 300 mg/kg in mice, 400 mg/kg in guinea pigs, and 300 mg/kg in rabbits. Acute exposure to lindane may lead to central nervous system stimulation (usually developing within 1 hour), mental/motor impairment, excitation, clonic (intermittent) and tonic (continuous) convulsion. Other adverse reactions include central nervous system toxicity, as well as skin and gastrointestinal changes.

Affected organisms
  • Scabies (Sarcoptes scabei) and other insects
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
No interactions found.
Food Interactions
Not Available

References

General References
  1. Brown VJ: Life after lindane in California. Environ Health Perspect. 2008 Mar;116(3):A128. [PubMed:18335087]
  2. Strong M, Johnstone P: Interventions for treating scabies. Cochrane Database Syst Rev. 2007 Jul 18;(3):CD000320. [PubMed:17636630]
External Links
Human Metabolome Database
HMDB14575
KEGG Drug
D00360
KEGG Compound
C07075
PubChem Compound
727
PubChem Substance
46508542
ChemSpider
10481896
BindingDB
50410525
ChEBI
32888
ChEMBL
CHEMBL15891
Therapeutic Targets Database
DAP001036
PharmGKB
PA164754914
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lindane
ATC Codes
P03AB02 — Lindane
MSDS
Download (54.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentLice of the head1

Pharmacoeconomics

Manufacturers
  • Reed and carnrick pharmaceuticals div block drug co inc
  • Sola barnes hind
  • Olta pharmaceuticals corp
  • Wockhardt eu operations (swiss) ag
  • Stiefel laboratories inc
Packagers
Dosage forms
FormRouteStrength
LiquidTopical1 %
ShampooTopical1 %
LotionTopical10 mg/mL
ShampooTopical10 mg/mL
LotionTopical1 %
Prices
Unit descriptionCostUnit
Lindane 1% Lotion 60ml Bottle142.33USD bottle
Lindane 1% Shampoo 60ml Bottle142.33USD bottle
Lindane 1% lotion5.16USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)112.5 °CPhysProp
boiling point (°C)323.4 °CPhysProp
water solubility7.3 mg/L (at 25 °C)RICHARDSON,LT & MILLER,DM (1960)
logP3.72HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00547 mg/mLALOGPS
logP3.94ALOGPS
logP4.35ChemAxon
logS-4.7ALOGPS
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity54.08 m3·mol-1ChemAxon
Polarizability23.08 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9918
Blood Brain Barrier+0.9862
Caco-2 permeable+0.8369
P-glycoprotein substrateNon-substrate0.8826
P-glycoprotein inhibitor INon-inhibitor0.9733
P-glycoprotein inhibitor IINon-inhibitor0.9944
Renal organic cation transporterNon-inhibitor0.8593
CYP450 2C9 substrateNon-substrate0.8522
CYP450 2D6 substrateNon-substrate0.7758
CYP450 3A4 substrateNon-substrate0.7335
CYP450 1A2 substrateInhibitor0.6037
CYP450 2C9 inhibitorNon-inhibitor0.7892
CYP450 2D6 inhibitorNon-inhibitor0.9592
CYP450 2C19 inhibitorNon-inhibitor0.5936
CYP450 3A4 inhibitorNon-inhibitor0.9007
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7408
Ames testNon AMES toxic0.9754
CarcinogenicityCarcinogens 0.5058
BiodegradationNot ready biodegradable0.9271
Rat acute toxicity2.0905 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9077
hERG inhibition (predictor II)Non-inhibitor0.9617
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (11.7 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - GC-EI-QGC-MSsplash10-00o0-4930000000-75eb17ef01463cc739eb
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as cyclohexyl halides. These are organohalogen compounds containing a monocyclic cyclohexane moiety that is substituted at one or more positions by an halogen atom.
Kingdom
Organic compounds
Super Class
Organohalogen compounds
Class
Alkyl halides
Sub Class
Cyclohexyl halides
Direct Parent
Cyclohexyl halides
Alternative Parents
Organochlorides / Hydrocarbon derivatives / Alkyl chlorides
Substituents
Cyclohexyl halide / Hydrocarbon derivative / Organochloride / Alkyl chloride / Aliphatic homomonocyclic compound
Molecular Framework
Aliphatic homomonocyclic compounds
External Descriptors
cyclodiene organochlorine insecticide, hexachlorocyclohexane (CHEBI:32888) / Organochlorine insecticides (C07075)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Cole LM, Roush RT, Casida JE: Drosophila GABA-gated chloride channel: modified [3H]EBOB binding site associated with Ala-->Ser or Gly mutants of Rdl subunit. Life Sci. 1995;56(10):757-65. [PubMed:7885191]
  4. Sauviat MP, Pages N: [Cardiotoxicity of lindane, a gamma isomer of hexachlorocyclohexane]. J Soc Biol. 2002;196(4):339-48. [PubMed:12645305]
  5. Anand M, Agrawal AK, Rehmani BN, Gupta GS, Rana MD, Seth PK: Role of GABA receptor complex in low dose lindane (HCH) induced neurotoxicity: neurobehavioural, neurochemical and electrophysiological studies. Drug Chem Toxicol. 1998 Feb;21(1):35-46. [PubMed:9530529]
  6. Joy RM, Walby WF, Stark LG, Albertson TE: Lindane blocks GABAA-mediated inhibition and modulates pyramidal cell excitability in the rat hippocampal slice. Neurotoxicology. 1995 Summer;16(2):217-28. [PubMed:7566682]
  7. Bloomquist JR: Chloride channels as tools for developing selective insecticides. Arch Insect Biochem Physiol. 2003 Dec;54(4):145-56. [PubMed:14635176]
  8. Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. [PubMed:8841090]
  9. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
  10. Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [PubMed:12614680]
  11. Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [PubMed:20600211]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA1
Uniprot ID
P23415
Uniprot Name
Glycine receptor subunit alpha-1
Molecular Weight
52623.35 Da
References
  1. Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [PubMed:12614680]
  2. Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [PubMed:20600211]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA2
Uniprot ID
P23416
Uniprot Name
Glycine receptor subunit alpha-2
Molecular Weight
52001.585 Da
References
  1. Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [PubMed:12614680]
  2. Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [PubMed:20600211]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA3
Uniprot ID
O75311
Uniprot Name
Glycine receptor subunit alpha-3
Molecular Weight
53799.775 Da
References
  1. Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [PubMed:12614680]
  2. Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [PubMed:20600211]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Glycine binding
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRB
Uniprot ID
P48167
Uniprot Name
Glycine receptor subunit beta
Molecular Weight
56121.62 Da
References
  1. Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [PubMed:12614680]
  2. Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [PubMed:20600211]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Gaba-gated chloride ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Ratra GS, Casida JE: GABA receptor subunit composition relative to insecticide potency and selectivity. Toxicol Lett. 2001 Jul 6;122(3):215-22. [PubMed:11489356]
  2. Chen L, Durkin KA, Casida JE: Structural model for gamma-aminobutyric acid receptor noncompetitive antagonist binding: widely diverse structures fit the same site. Proc Natl Acad Sci U S A. 2006 Mar 28;103(13):5185-90. Epub 2006 Mar 10. [PubMed:16537435]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Ratra GS, Erkkila BE, Weiss DS, Casida JE: Unique insecticide specificity of human homomeric rho 1 GABA(C) receptor. Toxicol Lett. 2002 Mar 24;129(1-2):47-53. [PubMed:11879973]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name
PGR
Uniprot ID
P06401
Uniprot Name
Progesterone receptor
Molecular Weight
98979.96 Da
References
  1. Scippo ML, Argiris C, Van De Weerdt C, Muller M, Willemsen P, Martial J, Maghuin-Rogister G: Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors. Anal Bioanal Chem. 2004 Feb;378(3):664-9. Epub 2003 Oct 25. [PubMed:14579009]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Scippo ML, Argiris C, Van De Weerdt C, Muller M, Willemsen P, Martial J, Maghuin-Rogister G: Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors. Anal Bioanal Chem. 2004 Feb;378(3):664-9. Epub 2003 Oct 25. [PubMed:14579009]
  2. Okubo T, Yokoyama Y, Kano K, Soya Y, Kano I: Estimation of estrogenic and antiestrogenic activities of selected pesticides by MCF-7 cell proliferation assay. Arch Environ Contam Toxicol. 2004 May;46(4):445-53. [PubMed:15253041]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
Molecular Weight
49761.245 Da
References
  1. Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [PubMed:16054614]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:37